发明授权
US08039612B2 Synthesis of oligonucleotides or phosphorothioate oligonucleotide with a capping agent of N-methylimidazole free of 1,3,5-trimethylhexahydro-1,3,5-triazine 有权
用不含1,3,5-三甲基六氢-1,3,5-三嗪的N-甲基咪唑封端剂合成寡核苷酸或硫代磷酸酯寡核苷酸

Synthesis of oligonucleotides or phosphorothioate oligonucleotide with a capping agent of N-methylimidazole free of 1,3,5-trimethylhexahydro-1,3,5-triazine
摘要:
According to the present invention, there is provided a process for making an oligonucleotide or a phosphorothioate oligonucleotide. The process has the following steps: (a) providing an amount of a blocked nucleotide; (b) deblocking the blocked nucleotide to form an unblocked nucleotide; (c) activating the deblocked nucleotide; (d) coupling the deblocked nucleotide with a phosphoramidite to form a phosphite oligomer; (e) capping any uncoupled deblocked nucleotide via reaction with an amount of acetic anhydride and an amount of N-methylimidazole that is substantially free of 1,3,5-trimethylhexahydro-1,3,5-triazine; (f) oxidizing the phosphite oligomer to form the oligonucleotide or sulfurizing the phosphite oligomer to form a phosphorothioate oligonucleotide; and (g) optionally repeating steps (b) through (f). There is also a process for capping a nucleotide.
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